Aqueous Dissolution and Dispersion Behavior of Polyvinylpyrrolidone Vinyl Acetate-based Amorphous Solid Dispersion of Ritonavir Prepared by Hot-Melt Extrusion with and without Added Surfactants.

摘要: Abstract In this study, the lack of complete drug release from amorphous solid dispersions (ASDs), as observed in most published reports, was investigated. ASDs with 20% ritonavir were prepared by HME using polyvinylpyrrolidone vinyl acetate (PVPVA) alone and combination 10% poloxamer 407 or Span 20 carriers. It established film casting technique that molecularly dispersed formulations, accelerated stability testing confirmed extrudates physically stable. Dissolution (100-mg equivalent) performed 250 mL 0.01 N HCl (pH 2), pH 6.8 phosphate buffer FeSSIF-V2. Drug concentrations measured filtration through 0.45-μm pores unfiltered media; latter gave total amounts present dissolution media, both solution dispersion. Because low solubility, did not dissolve completely aqueous media. Rather, it formed supersaturated solutions, excess oily form particle sizes could crystallize time. Due to higher dissolved FeSSIF-V2 much than buffer. Complete be accounting for phase-separated Thus, study provides a picture in vitro dispersion ASDs.